759415-90-2Relevant academic research and scientific papers
Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus
McGowan, David,Herschke, Florence,Pauwels, Frederik,Stoops, Bart,Last, Stefaan,Pieters, Serge,Scholliers, Annick,Thoné, Tine,Van Schoubroeck, Bertrand,De Pooter, Dorien,Mostmans, Wendy,Khamlichi, Mourad Daoubi,Embrechts, Werner,Dhuyvetter, Deborah,Smyej, Ilham,Arnoult, Eric,Demin, Samu?l,Borghys, Herman,Fanning, Gregory,Vlach, Jaromir,Raboisson, Pierre
, p. 7936 - 7949 (2016/11/07)
Toll-like receptor (TLR) 7 and 8 agonists can potentially be used in the treatment of viral infections and are particularly promising for chronic hepatitis B virus (HBV) infection. An internal screening effort identified a pyrimidine Toll-like receptor 7 and 8 dual agonist. This provided a novel alternative over the previously reported adenine and pteridone type of agonists. Structure-activity relationship, lead optimization, in silico docking, pharmacokinetics, and demonstration of ex vivo and in vivo cytokine production of the lead compound are presented.
Discovery of (S)-4-isobutyloxazolidin-2-one as a novel leucyl-tRNA synthetase (LRS)-targeted mTORC1 inhibitor
Yoon, Suyoung,Kim, Jong Hyun,Yoon, Ina,Kim, Changhoon,Kim, Sung-Eun,Koh, Yura,Jeong, Seung Jae,Lee, Jiyoun,Kim, Sunghoon,Lee, Jeewoo
, p. 3038 - 3041 (2016/06/13)
A series of leucinol analogs were investigated as leucyl-tRNA synthetase-targeted mTORC1 inhibitors. Among them, compound 5, (S)-4-isobutyloxazolidin-2-one, showed the most potent inhibition on the mTORC1 pathway in a concentration-dependent manner. Compound 5 inhibited downstream phosphorylation of mTORC1 by blocking leucine-sensing ability of LRS, without affecting the catalytic activity of LRS. In addition, compound 5 exhibited cytotoxicity against rapamycin-resistant colon cancer cells, suggesting that LRS has the potential to serve as a novel therapeutic target.
PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
-
Page/Page column 50, (2012/10/18)
This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
